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α-Glucosidase inhibition of 6-hydroxyflavones. Part 3, Synthesis and evaluation of 2,3,4-trihydroxybenzoyl-containing flavonoid analogs and 6-aminoflavones as α-previous termglucosidasenext term inhibitors

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Title: α-Glucosidase inhibition of 6-hydroxyflavones. Part 3, Synthesis and evaluation of 2,3,4-trihydroxybenzoyl-containing flavonoid analogs and 6-aminoflavones as α-previous termglucosidasenext term inhibitors
Authors: Gao, Hong Browse this author
Kawabata, Jun2 Browse this author →KAKEN DB
Authors(alt): 川端, 潤2
Keywords: α-previous termGlucosidase
structure-activity relationship
6-hydroxyflavones
6-aminoflavones
Issue Date: 1-Mar-2005
Publisher: Elsevier
Journal Title: Bioorganic & Medicinal Chemistry
Volume: 13
Issue: 5
Start Page: 1661
End Page: 1667
Publisher DOI: 10.1016/j.bmc.2004.12.010
PMID: 15698784
Abstract: The SAR studies suggested that the C-ring of baicalein (1) was not necessary for the activity, and validated the importance of 2,3,4-trihydroxybenzoyl structure of 1. Thus, a series of 2,3,4-trihydroxybenzoyl-containing flavonoid analogs were investigated for the α-previous termglucosidasenext term inhibitory activity. The results indicated that 5,6,7-trihydroxy-2-phenyl-4-quinolone (2) and 5,6,7-trihydroxyflavanone (4) showed the comparable activity to 1, while 3,5,6,7-tetrahydroxyflavone (7), 5,6,7-trihydroxyisoflavone (8), and 6-hydroxygenistein (9) showed moderate α-previous termglucosidasenext term inhibitory activity. In addition, it was found that 6-amino-5,7-dihydroxyflavone (16) was a more potent and specific rat intestinal α-previous termglucosidasenext term inhibitor than 1, and showed the comparable activity to acarbose. This is the first report on mammalian intestinal α-previous termglucosidasenext term inhibitory activity of 6-aminoflavones. Kinetic studies revealed that 16 inhibited both sucrose- and maltose-hydrolyzing activities of rat intestinal α-previous termglucosidasenext term uncompetitively.
Relation: http://www.sciencedirect.com/science/journal/09680896
Type: article (author version)
URI: http://hdl.handle.net/2115/433
Appears in Collections:農学院・農学研究院 (Graduate School of Agriculture / Faculty of Agriculture) > 雑誌発表論文等 (Peer-reviewed Journal Articles, etc)

Submitter: 川端 潤

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